WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 555805
Description: NE52-QQ57 is an orally available GPR4 antagonist with an IC50 of 70 nM. NE 52-QQ57 significantly inhibited the AGE-induced increased expression of several key inflammatory cytokines and signaling molecules, including tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, IL-6, inducible nitric oxide synthase (iNOS), nitric oxide (NO), cyclooxygenase 2 (COX2), and prostaglandin E2 (PGE2).
MedKoo Cat#: 555805
Name: NE 52-QQ57
Chemical Formula: C24H28N6O
Exact Mass: 416.2325
Molecular Weight: 416.529
Elemental Analysis: C, 69.21; H, 6.78; N, 20.18; O, 3.84
Synonym: NE52-QQ57; NE-52-QQ57; NE 52-QQ57; NE52QQ57; NE-52QQ57; NE 52QQ57;
IUPAC/Chemical Name: 2-(4-((2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl)phenyl)-5-(piperidin-4-yl)-1,3,4-oxadiazole
InChi Key: HXPQWNPLNIEJOW-UHFFFAOYSA-N
InChi Code: InChI=1S/C24H28N6O/c1-4-21-20(22-26-15(2)13-16(3)30(22)29-21)14-17-5-7-18(8-6-17)23-27-28-24(31-23)19-9-11-25-12-10-19/h5-8,13,19,25H,4,9-12,14H2,1-3H3
SMILES Code: CCC1=NN(C(C)=CC(C)=N2)C2=C1CC3=CC=C(C4=NN=C(C5CCNCC5)O4)C=C3
Osteoarthritis (OA) is a common degenerative joint disease for which an effective therapeutic strategy has not yet been established. AGEs are widely recognized as a contributor to OA pathogenesis. GPR4, a recently discovered proton-sensing transmembrane receptor, has been shown to possess a wide range of physiological functions. However, the potential role of this receptor in chondrocytes and the pathogenesis of OA is unclear.
1: Liu H, Liu Y, Chen B. Antagonism of GPR4 with NE 52-QQ57 and the Suppression of AGE-Induced Degradation of Type II Collagen in Human Chondrocytes. Chem Res Toxicol. 2020 May 18. doi: 10.1021/acs.chemrestox.0c00111. Epub ahead of print. PMID: 32370492.
2: Hosford PS, Mosienko V, Kishi K, Jurisic G, Seuwen K, Kinzel B, Ludwig MG, Wells JA, Christie IN, Koolen L, Abdala AP, Liu BH, Gourine AV, Teschemacher AG, Kasparov S. CNS distribution, signalling properties and central effects of G-protein coupled receptor 4. Neuropharmacology. 2018 Aug;138:381-392. doi: 10.1016/j.neuropharm.2018.06.007. Epub 2018 Jun 9. PMID: 29894771; PMCID: PMC6063991.